Other countries, such as Armenia, Russia, and Ukraine classify it as a psychotropic substance while some, such as Spain (brand name Zinosal), have no restrictions on its use. Tianeptine is not approved in Australia, Canada, New Zealand, or the United Kingdom. In 2024, the FDA urged convenience stores and gas stations to stop selling Neptune’s Fix or any products with tianeptine. At higher doses, tianeptine products linked to serious harm, overdoses, death tianeptine starts affecting dopamine levels in addition to serotonin. This important hormone can contribute to addictive behavior by changing neural connectivity to reinforce an activity that brings feelings of pleasure and euphoria. The drug increases opioid activity in the brain, a similar mechanism of action seen in heroin.
- There are also reports of at least five fatal overdoses since the drug started being sold in the US.
- Poison control center cases involving tianeptine exposure have increased nationwide, from 11 total cases between 2000 and 2013 to 151 cases in 2020 alone.
- Tianeptine’s effectiveness in treating depression is of clinical, as well as conceptual, significance.
- Tianeptine works on chemicals within the brain such as serotonin and at low doses can affect mood.
- In some cases, those laws have led to more cases of withdrawal among users of tianeptine, which can be chemically addictive.
Tianeptine: An Antidepressant with Memory-Protective Properties
Quantitation was performed through liquid chromatography-tandem mass spectrometry (LC-MS-MS) using a binary gradient of 0.1% formic acid in water and 0.1% formic acid in acetonitrile. The authors noted the difficulty in recovering tianeptine because it comprises both active acidic and basic groups. However, fragmentation was not impeded, and two ion transitions were successfully acquired.
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Several case reports showed that tianeptine toxicity mimicked opioid toxicity and that naloxone was an effective therapy (6,7). Neonatal abstinence syndrome mimicking opioid neonatal abstinence syndrome has occurred after tianeptine dependence during pregnancy (9). This study further highlights that the withdrawal effects of tianeptine mimic those of opioid withdrawal. “Case reports in the medical literature describe U.S. consumers ingesting daily doses on the order of 1.3 to 250 times (50 mg to 10,000 mg) the daily tianeptine dose typically recommended in labeled foreign drug products,” the letter read. Many tianeptine products claim— without evidence or FDA approval— to help users treat medical conditions, including addiction, pain and depression. Tianeptine is often marketed as all-natural, which makes it hard for people to grasp its dangers, especially when it is sold so freely in roadside stores.
He ultimately increased use to a dose of 150 mg three or four times daily, noting a brief sensation of euphoria after administration. A urine drug screen was positive for barbiturates, which was thought to be an adulterant. The authors warn of an increased risk of tianeptine adulterants in the United States, citing lack of regulation, and raise concerns over the potentially life-threatening side effects when administered alongside sedatives 23. As its pharmacology has been elucidated over the past several years, namely its activity at the opioid receptor, there has been a growing interest in tianeptine misuse in the United States 6. Despite lacking FDA approval for any purpose in the United States, tianeptine can still be found in certain convenience stores and gas stations 6.
Although the FDA has warned consumers about tianeptine, vendors continue to market and sell tianeptine for medical uses. Other symptoms include agitation, confusion, sweating, nausea, vomiting, drowsiness and coma. In some cases, those laws have led to more cases of withdrawal among users of tianeptine, which can be chemically addictive. Experts aren’t sure but national figures show a big rise in emergency calls involving the drug. People quickly develop a tolerance to tianeptine which causes them to increase how much they take, which is a clear sign of addiction and dependence. To stop themselves from going into withdrawal, some set an alarm to wake themselves up every two hours to take their tianeptine pills.
Additionally, the same chronic stress that leads to hypertrophy of cells in the amygdala increases the expression of anxiety-like behaviors in rats tested in the elevated plus maze 197,198. In general, studies have reported significant reductions of hippocampal and prefrontal cortex volumes in depressed patients 74,111,194. The hippocampus is a medial temporal lobe structure which is important for declarative memory in humans 49,182 and spatial working memory in rodents 20,21,79,128,129,207. The prefrontal cortex is located in the anterior portion of the frontal lobe and plays an important role in complex cognitive processes, such as planning, decision-making and behavioral flexibility 13. Depressed individuals exhibit impaired performance on hippocampus- and prefrontal cortex-dependent cognitive tasks, which corresponds with reduced or abnormal activity in each of these brain regions when depressed patients engage in such tasks 47,126.
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But about a dozen states have passed laws prohibiting or restricting tianeptine, including Alabama, Georgia, Michigan, Minnesota, Ohio and Tennessee. While tianeptine is not an opioid, the drug binds to some of the same receptors in the brain, which can temporarily produce effects akin to oxycodone and other opioids. Tianeptine also carries some of the same physiological risks of opioids, including the potential to dangerously depress breathing. Overseas, tianeptine was reclassified in France in 2012 as a narcotic after an analysis determined that the benefits of using the drug for depression did not outweigh the risks.
North Carolina Bans ‘Gas Station Heroin’
Tianeptine is an antidepressant drug that is not approved by the Food and Drug Administration (FDA). Clinical effects of tianeptine abuse and withdrawal can mimic opioid toxicity and withdrawal. Uzbay and colleagues found that tianeptine reduced the intensity 27 and delayed the onset 192 of pentylenetetrazole-induced seizures in rodents.
First author, MQ, received a student scholar research stipend from the Child Injury Prevention Alliance while he worked on this study. The interpretations and conclusions in this article do not necessarily represent those of the funding organization. The funding organization was not involved in the design and conduct of the study; collection, management, analysis, and interpretation of the data; preparation, review, or approval of the manuscript; and decision to submit the manuscript for publication. All authors have completed and submitted the International Committee of Medical Journal Editors form for disclosure of potential conflicts of interest.
Systematic Review of Clinical Case Reports Involving Tianeptine Products: “Gas Station Heroin” Hype or Fact?
- Given the rapidity, reliability, low cost, and high sensitivity of the test, it is suggested that it may help analyze biological samples in the clinical setting 27.
- “While the FDA is closely following the distribution and sale of these products, it is critical that you appreciate the magnitude of the underlying danger of these products, and disseminate information about it.”
- Second, we were able to obtain confirmatory analytic testing on only a small number of the total cases, and contents identified in these product samples may not be generalizable to all patients in the outbreak.
- Tianeptine, which is often called “gas station heroin” because of its availability in gas station stores, is not approved by the FDA for any use.
Because of its high potential for drug abuse, those who regularly misuse the pills may exhibit withdrawal symptoms such as stomachaches and anxiety if they try to quit. Consumers are usually taking a gamble when they buy tianeptine products because they can’t know for sure how much of the drug they’re getting. This increases the risk of an unintentional overdose, along with other adverse side effects like lethargy, elevated blood pressure and heart rate, agitation, abdominal pain, tremors, and hallucinations. Tianeptine, an atypical antidepressant not approved in the United States, is readily purchased from unregulated markets such as the internet and gas stations. We became aware of a cluster of 34 patients in New Jersey who became ill following ingestion of the tianeptine containing-product Neptune’s Fix, the rate of which (4.6 cases per month) far exceeded the background rate for this substance of 0.5 cases per year.
Gas Station Treatment History and Relation to Tianeptine
As a full agonist, it produces a euphoric high and carries a significant risk of overdose. Furthermore, its short half-life can lead to rapid withdrawal, increasing its potential for addiction and misuse. This study demonstrates the toxicity and rapid increase of tianeptine exposures reported to US poison centers. Uniform regulation of tianeptine across all states may offer an important strategy to help mitigate this public health problem. In the U.S., reports of bad reactions and unwanted effects involving tianeptine are increasing. Annual poison control center cases involving tianeptine exposure, as reported by the National Poison Data System, have increased nationwide, from 4 cases in 2013 to about 350 cases in 2024.
Acute Toxicity Following Tianeptine Ingestion
No human subjects/ data were involved in the construction of this manuscript outside of the original studies in this review. A .gov website belongs to an official government organization in the United States. The .gov means it’s official.Federal government websites often end in .gov or .mil.